382187

HDAC Inhibitor XXIII, Tubastatin A

The HDAC Inhibitor XXIII, Tubastatin A controls the biological activity of HDAC. This small molecule/inhibitor is primarily used for Cell Structure applications.

• Sinónimos: HDAC Inhibitor XXIII, Tubastatin A, N-Hydroxy-4-(2-methyl-1,2,3,4-tetrahydro-pyrido[4,3-b]indol-5-ylmethyl)benzamide
• Fórmula empírica (notación de Hill): C₂₀H₂₁N₃O₂
• Peso molecular: 335.40
• Código UNSPSC: 12352200
• NACRES: NA.28

Propiedades

• Nivel de calidad: 100
• Análisis: ≥95% (HPLC)
• formulario: solid
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; desiccated (hygroscopic); protect from light
• color: tan
• solubilidad: DMSO: 10 mg/mL; ethanol: 250 μg/mL
• Condiciones de envío: ambient
• temp. de almacenamiento: −20°C

Descripción

Descripción general

A cell-permeable carbazolohydroxamate that acts as a highly potent HDAC6-selective inhibitor (IC₅₀ = 15 nM) with much reduced or no activity against other known HDACs. Effectively prevents neuronal cell death (by ≥95% at 10 µM) upon oxidative stress induction by HCA and selectively induces cellular α-tubulin, but not histone H4, hyperacetylation (2.5 to 5 µM) in primary rat cortical neuron cultures.

A cell-permeable carbazolohydroxamate whose zinc-chelating hydroxamic acid moiety and catalytic channel rim-targeting aromatic cap structure render it a highly potent HDAC6-selective inhibitor (IC₅₀ = 15 nM against recombinant human HDAC6) with much reduced or no activity against HDAC8, HDAC1 (IC₅₀ = 0.854 and 16.4 µM, respectively), and other known HDACs (HDAC2/3/4/5/7/9/10/11; IC₅₀ >30 µM). Shown to selectively block HDAC6-, but not HDAC1-, dependent cellular deacetylation as evidenced by its selective induction (2.5 to 5 µM) of α-tubulin, but not histone H4, hyperacetylation in cultured primary rat cortical neurons. Although failing to block cellular glutathione depletion by homocysteic acid (HCA), Tubastatin A nevertheless is reported to prevent neuronal cell death upon oxidative stress induction by HCA in a dose-dependent manner (≥95% protection at 10 µM), presumably by preventing peroxiredoxins deacetylation.

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Otras notas

Butler, K.V., et al. 2010. J. Am. Chem. Soc.132, 10842.

Información legal

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 2
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable